N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors

…, JR Tonra, S Mitelman, MM Camara, DS Deevi…

Index: Xu, Yong-Jiang; Miao, Hua-Quan; Pan, Weitao; Navarro, Elizabeth C.; Tonra, James R.; Mitelman, Stan; Camara, M. Margarita; Deevi, Dhanvanthri S.; Kiselyov, Alexander S.; Kussie, Paul; Wong, Wai C.; Liu, Hu Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 404 - 408

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Citation Number: 19

Abstract

A novel class of N-(4-{[4-(1H-benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamides are described as inhibitors of the endo-β-glucuronidase heparanase. Among them are N-(4- {[4-(1H-benzoimidazol-2-yl)-phenylamino]-methyl}-phenyl)-3-bromo-4-methoxy-benzamide (15h), and N-(4-{[5-(1H-benzoimidazol-2-yl)-pyridin-2-ylamino]-methyl}-phenyl)-3-bromo-4- methoxy-benzamide (23) which displayed good heparanase inhibitory activity (IC50 0.23– ...

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